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Method for preparing epirubicin slow-release prepn

A technology of epirubicin and sustained-release microspheres, which is used in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. It can solve the problem that epirubicin is unstable and can only be stored. problems, to achieve the effects of improved drug release characteristics, high encapsulation efficiency, and simple operation process

Active Publication Date: 2011-01-26
瀚晖制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Epirubicin is a commonly used anti-tumor chemotherapy drug. Its main function is to directly intercalate between DNA base pairs, interfere with the transcription process, and prevent the formation of mRNA, thereby inhibiting the growth of tumor cells. It has certain anti-tumor activity, but its effect on The human body also has strong bone marrow suppression and cardiotoxicity. In addition, epirubicin is unstable at high temperature and high humidity, and the drug can only be stored at room temperature for 24 hours after dissolution.

Method used

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  • Method for preparing epirubicin slow-release prepn
  • Method for preparing epirubicin slow-release prepn
  • Method for preparing epirubicin slow-release prepn

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] (1) Dissolve 5 mg of epirubicin hydrochloride in 30 ml of N-N dimethylformamide (DMF) to obtain solution A; (2) take 10 μl of triethylamine and add it to solution A to obtain solution B; (3) weigh 50 mg of polylactic acid (relative molecular weight is 5000) was added to solution B to obtain solution C; (4) 1.6 ml of water was added to solution C to obtain a turbid solution; (5) the turbid solution was transferred to a dialysis bag, and the dialysis Place the bag in distilled water for dialysis, stir at the same time, and change the water every 2 hours; (6) After 8 hours, centrifuge the product obtained in step 5, sonicate, and wash 3 times with water to remove unembedded epirubicin, and take the sample obtained by freeze-drying the precipitate . The encapsulation efficiency of the obtained sample was 59.6%, and the drug loading rate was 6.8%. The surface of the microspheres was observed through a scanning electron microscope to be smooth, and the particle size distribut...

Embodiment 2

[0026] (1) Dissolve 12 mg of epirubicin hydrochloride in 18 ml of N-N dimethylformamide (DMF) to obtain solution A; (2) take 12 μl of triethylamine and add it to solution A to obtain solution B; (3) weigh Add 60mg of polylactic acid (relative molecular weight: 5000) to solution B to obtain solution C; (4) add 2ml of pure water to solution C to obtain a cloudy solution; (5) transfer the cloudy solution to a dialysis bag (8000-14000 ), and place the dialysis bag in distilled water for dialysis, while stirring, and change the water every 2h; (6) after 24h, the product obtained in step 5 is centrifuged, ultrasonicated, and washed 3 times with water to remove unembedded epirubicin, and take The resulting sample was precipitated and freeze-dried. The encapsulation rate of the obtained sample was 53.6%, and the drug loading rate was 7.4%. The scanning electron microscope observed that the surface of the microspheres was smooth, and the particle size distribution was between 200nm and...

Embodiment 3

[0028] (1) 4 mg of epirubicin hydrochloride was dissolved in 3 ml of N-N dimethylformamide (DMF) to obtain solution A; (2) 2 μl of triethylamine was added to solution A to obtain solution B; (3) weighed Add 40mg of polylactic acid (relative molecular weight is 10,000) into solution B to obtain solution C; (4) add 0.75ml of pure water to solution C to obtain a cloudy solution; (5) transfer the cloudy solution to a dialysis bag (8000 ~14000), put the dialysis bag in distilled water for dialysis, stir at the same time, change the water every 2h; (5) after 4h, centrifuge the product obtained in step 5, ultrasonic, and wash 3 times with water to remove unembedded epirubicin , take the sample obtained by freeze-drying the precipitate. The encapsulation efficiency of the obtained sample was measured to be 30.9%, and the drug loading rate was 4.9%. The scanning electron microscope observed that the surface of the microspheres was smooth, and the particle size distribution was between ...

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Abstract

A slow-release epidoxorubicin-polylactic acid microball is prepared through dissolving epidoxorubicin hydrochloride in DMF, adding triethylamine, adding polylactic acid, adding water, dialyzing in water while stirring and exchanging water every 1-3 hr, centrifugal dewatering, ultrasonic treating, water washing, removing uncoated epidoxorubicin, and freeze-drying of deposit.

Description

technical field [0001] The invention relates to a drug-loaded polymer microsphere, in particular to a preparation method of a polylactic acid sustained-release preparation loaded with epidoxorubicin. Background technique [0002] Polylactic acid (PLA) has been widely used in sustained drug release due to its good biocompatibility and biodegradability, and has become one of the most valued materials in biodegradable medical materials. At present, the preparation methods of polylactic acid drug-loaded microspheres mainly include phase separation method, emulsification solvent evaporation method, spray method and so on. Among them, the emulsified solvent evaporation method is the most widely used. The emulsification-solvent evaporation method is to dissolve the polymer in an organic solvent, and then emulsify it in an aqueous solution under stirring. With the evaporation of the solvent, polymer microspheres are formed slowly. This type of method uses a large amount of surfact...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K47/34A61P35/00
Inventor 张其清刘敏翁建叶社房
Owner 瀚晖制药有限公司
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